LAG-3 Binding Peptides for Cost-Effective Cancer Immunotherapy
Find Innovative SolutionsGenerate Solutions
Solution Overview
Problem
Current cancer immunotherapy methods targeting LAG-3/MHC class II interactions show limited efficacy in many patients, and there is a need for more effective inhibitors to enhance immune cell function against cancer cells.
Innovation Solution
Development of peptides (LAG3Pep-1 and LAG3Pep-2) that specifically bind to LAG-3, inhibiting its function and activating immune cells, combined with a PD-L1 antibody for enhanced cancer treatment.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If monoclonal antibodies targeting LAG-3 are used to block LAG-3/MHC class II interactions, then immune cell function is activated and antitumor responses are improved, but treatment cost increases and accessibility decreases
Solution Approach 1:
The patent replaces expensive monoclonal antibodies with small peptide molecules (10-50 amino acids) that can be synthesized chemically at much lower cost. These peptides block LAG-3 function temporarily but can be administered repeatedly, providing a cost-effective alternative to long-lasting antibody therapy
Solution Approach 2:
The invention changes the molecular size parameter from large antibody molecules (150 kDa) to small peptide molecules (1-5 kDa), enabling cheaper production through chemical synthesis while maintaining the ability to block LAG-3/MHC class II interactions and activate immune cells
2Reliability
If LAG-3 blocking therapy is administered alone, then some antitumor effect is achieved, but response rate remains limited in many patients
Solution Approach 1:
The patent combines LAG-3 blocking peptides with PD-L1 blocking antibodies in a single therapeutic regimen. This combination therapy targets multiple immune checkpoint pathways simultaneously (LAG-3 and PD-L1), overcoming resistance to monotherapy and increasing overall response rate in cancer patients
Solution Approach 2:
The therapeutic composition serves multiple functions: the peptide component blocks LAG-3/MHC class II interactions to activate T cells, while the antibody component blocks PD-L1 to prevent immune evasion. This multi-functional approach addresses different mechanisms of immune suppression in a single treatment
Applied Scientific Principles
This section explains which scientific principles are used to turn an abstract innovation direction into a practical engineering solution.
Function Achieved in This Case
The peptides exhibit anticancer effects by activating immune cells, similar to antibodies, and when co-administered with a PD-L1 antibody, demonstrate significant tumor growth inhibition in mouse models.
Implementation Method 1
The peptide of the present disclosure was obtained via a phage peptide display technology by targeting a cell in which a human LAG-3 protein is highly expressed to select two types of peptides (LAG3Pep-1 and LAG3Pep-2) that well bind to the cell
Data Source
Figure 1A~1C
Figure 2A~2D
Figure 3A~3D
AI summary
The present invention relates to peptides binding to LAG-3 and a use thereof in cancer immunotherapy and anticancer applications. The peptides of the present invention specifically bind to and inhibit LAG-3, thereby activating the function of immune cells against cancer cells and exhibiting anticancer effects. Using phage peptide display technology targeting cells with high expression of human LAG-3 protein, two peptides, LAG-3Pep-1 and LAG-3Pep-2, which were found to highly bind to the protein, were selected as the peptides of the present invention. These peptides were confirmed to bind to both human and mouse LAG-3 and inhibit its function. The peptides of the present invention showed effects similar to those of antibodies and were relatively stable in the bloodstream, indicating high potential as future cancer immunotherapeutics.